- A concise synthesis of atipamezole
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Atipamezole (1), a potent α2 adrenergic receptor antagonist, was synthesized in four steps from dibromide 2 and 2,4-pentanedione.
- Wong,Gluchowski
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- A class of indoleamine 2,3-dioxygenase regulating compound and uses in pharmacy
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The invention relates to compounds, which are one or a variety of inhibitors of indoleamine 2,3-dioxygenase. The invention further provides a pharmaceutical component containing the compound, a preparation containing the compound, and uses of the indoleamine 2,3-dioxygenase inhibitors, wherein the indoleamine 2,3-dioxygenase inhibitors can be separately used or can be combined with other drugs soas to treat symptoms related to indoleamine 2,3-dioxygenase.
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Paragraph 0250; 0267; 0268; 0269; 0270
(2018/09/08)
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- An unexpected directing effect in the asymmetric transfer hydrogenation of α,α-disubstituted ketones
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α,α-Disubstituted ketones containing an aromatic ring or alkene are reduced in high enantiomeric excess using an asymmetric transfer hydrogenation catalyst. The sense of reduction indicates that the unsaturated region of the ketone adopts a position adjacent to the Ru-bound η6-arene ring in the reduction transition state.
- Soni, Rina,Collinson, John-Michael,Clarkson, Guy C.,Wills, Martin
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supporting information; experimental part
p. 4304 - 4307
(2011/10/11)
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- α,β-Epoxy Sulfoxides as Useful Intermediates in Organic Synthesis. X. An Improved Synthesis of α,β-Unsaturated Carbonyl Compounds from Carbonyl Compounds with Carbon Homologation through α,β-Epoxy Sulfoxides
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Treatment of the α,β-epoxy sulfoxides derived from ketones and chloromethyl phenyl sulfoxide or 1-chloroalkyl phenyl sulfoxides with lithium perchlorate in the presence of tributylphosphine oxide in toluene at 110 deg C for about 1-3 h gave α,β-unsaturated aldehydes or α,β-unsaturated ketones in high yields.In contrast to these results, the α,β-epoxy sulfoxides derived from aldehydes did not give the desired α,β-unsaturated ketones.In this case, a sequential treatment of the α,β-epoxy sulfoxides with benzenethiolate and m-chloroperbenzoic acid afforded α-phenylsulfinylated ketones, which were heated in toluene at 110 deg C to give the desired enones in good overall yields.The oxidation of the α,β-unsaturated aldehydes obtained by this method gave α,β-unsaturated carboxylic acids in high yields.These procedures afforded a new method for the synthesis of α,β-unsaturated carbonyl compounds, including α,β-unsaturated esters, from carbonyl compounds with carbon homologation.
- Satoh, Tsuyoshi,Itoh, Masayuki,Ohara, Teruhiko,Yamakawa, Koji
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p. 1839 - 1846
(2007/10/02)
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